货号：E2389

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

The androgen receptor (AR), also known as NR3C4, is one kind of nuclear receptor. When binding either of androgenic hormones, testosterone or dihydrotestosterone, androgen receptor can be activated and translocate into the nucleus. Increased androgen receptor gene expression may critically influence cancer progression such as, prostate cancer. Enzalutamide, also called as MDV3100, is an androgen-receptor (AR) antagonist with IC50 of 36 nM (measured by relative AR binding affinity). Enzalutamide can prevent nuclear translocation and impair DNA binding of AR induced by R1881 (a synthetic androgen), which facilitated mediating reduced PSA levels in AR-positive prostate cancer cell line (LNCaP) and inhibiting the growth of LNCaP cells. Enzalutamide is the first approved second-generation androgen receptor (AR) antagonist in the treatment of metastatic castration-resistant prostate cancer (mCRPC) and shows good pharmacokinetic profiles in human as well as animal.

作用机制
Enzalutamide is a competitive inhibitor of AR ligand binding.

产品信息